Synthesis, anti-proliferative activity, SAR, and kinase inhibition studies of thiazol-2-yl- substituted sulfonamide derivatives
作者:Chandrakant D. Pawar、Sadhana L. Chavan、Umakant D. Pawar、Dattatraya N. Pansare、Santosh V. Deshmukh、Devanand B. Shinde
DOI:10.1002/jccs.201800312
日期:2019.3
A series of novel thiazol‐2‐yl substituted‐1‐sulfonamide derivatives were synthesized from anilines. This involved the coupling of sulfonyl chlorides with thiazol amine to obtain the final compounds 7a–7j and 8a–8j. All synthesized compounds were screened for anticancer activity against MCF‐7, HeLa, A‐549, and Du‐145 cancer cell lines by 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide
从苯胺合成了一系列新颖的噻唑-2-基取代的1-磺酰胺衍生物。这涉及将磺酰氯与噻唑胺偶联以获得最终化合物7a – 7j和8a – 8j。通过3-(4,5-二甲基噻唑-2-基)-2-5-二苯基四唑溴化物(MTT)筛选所有合成的化合物对MCF-7,HeLa,A-549和Du-145癌细胞的抗癌活性分析。初步的生物测定表明,大多数化合物均表现出不同程度的抗增殖作用,阿霉素可用作阳性对照。在不同的细胞系中,合成的化合物显示的IC 50值为2.74–8.17μM。化合物7d,7e与阿霉素相比,,8a,8d和8e的活性更高。具有丁基和潘基链的化合物比其低级和高级碳链以及其环对应物更具活性。